Nedocromil Sodium Ophthalmic Solution - Indication, Dosage, and Side Effects

Overview:

Nedocromil sodium ophthalmic solution is used to treat itchy eyes caused by allergies. Nedocromil works by decreasing the release of natural substances, which are formed due to an allergic reaction. Nedocromil is a pyrroloquinoline derivative that blocks the activation of inflammatory cells formed due to allergic reactions like asthma, including the eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets.

What Are the Indications for Nedocromil Sodium Ophthalmic Solution?

Indications for Nedocromil sodium ophthalmic solution is to treat itchiness associated with allergic conjunctivitis.

Dosage:

• Dosage Form: Solution.

• Dosage Strength: 2 %; Five milliliters of solution in a ten-milliliter bottle.

• Supplied: Nedocromil sodium ophthalmic solution is supplied in a natural, low-density polyethylene round eye drop bottle with a dropper tip.

• Storage: It is stored at 2-degree to 25-degree Celsius but in tightly closed bottles.

• Recommended Dosage: One to two drops in each eye is recommended twice a day and used in regular intervals.

What Are the Contraindications to Nedocromil Sodium Ophthalmic Solution?

Contraindications for Nedocromil sodium ophthalmic solution is for those patients who are hypersensitive to Nedocromil sodium or the other ingredients.

What Are the Precautions While Using Nedocromil Sodium Ophthalmic Sodium?

Precautions while using the Nedocromil sodium ophthalmic are:

• Patients who are using contact lenses should avoid wearing lenses while having signs of itchy eyes or allergic conjunctivitis.

What Are the Special Considerations for Nedocromil Sodium Ophthalmic Solution?

Special considerations for Nedocromil sodium solution are:

• Pregnancy: The studies on animals like mice, rats, and rabbits have shown no teratogenicity effects with no harm to the fetus because of the use of Nedocromil sodium ophthalmic solution. The study was performed on mice and rats by using a subcutaneous dose of 100 milligrams per kilogram per day, which is usually 1600 times more dose delivered to humans and has presented no teratogenic effects on these animals. But still, there are no studies that have evidence that proves the safety of Nedocromil sodium use on pregnant women. So, Nedocromil sodium is used cautiously in pregnancy, and the use of Nedocromil sodium in pregnancy should be done if it is required.

• Nursing Mothers: It was studied on the animals that the Nedocromil sodium ophthalmic solution is excreted in milk. But still, it is not sure whether the Nedocromil sodium solution is excreted in human breast milk or not. So, the cautious use of Nedocromil sodium is done in nursing mothers and recommended to nursing mothers only if it is needed.

• Pediatric Use: The safety and the effectiveness of the Nedocromil sodium ophthalmic solution are not determined in children below the age of three.

• Geriatric Use: The safety and effectiveness of Nedocromil sodium ophthalmic solution are not determined in elderly patients. So, it is used by the elderly cautiously.

For Patients:

What Is the Use of Nedocromil Sodium Ophthalmic Solution?

Nedocromil sodium ophthalmic solution is used to treat itchy eyes caused by allergies. There are symptoms that develop due to allergies, as mast cells present in the body for immunity get released on allergic reactions. So, here the use of Nedocromil is a medicine that belongs to the class of mast cell stabilizers that works by inhibiting the release of these mast cells.

How Is the Nedocromil Sodium Ophthalmic Solution Used?

The Nedocromil sodium ophthalmic solution comes in the form of a solution to instill in the eyes. It is used to instill twice a day. It should be used as directed by the doctor. It should be used as recommended by the doctor, not too more or less should be instilled. The symptoms of itchy eyes usually improve on instilling Nedocromil sodium. Still, if there are no improvements in the signs or symptoms and if the symptoms get worse, then the patient should consult the doctor. The patient should continue using the Nedocromil sodium even after the improvement of symptoms. It should be discontinued after consulting the doctor.

How to Instill Nedocromil Sodium?

Steps to instill Nedocromil sodium ophthalmic solution is:

• Wash the hands thoroughly with soap and water.

• Check the dropper tip.

• The patient should avoid touching the dropper tip by keeping it against the eye. However, the eye drops and droppers are kept clean.

• The patient should tilt the head back and pull down the eye's lower lid with the help of the index finger to form the pocket.

• The dropper should be held with the other hand near the eye without touching it.

• The patient braced the remaining fingers of the hand against the face.

• Looking up, start squeezing the dropper so that a single drop falls into the pocket that is made by the lower eyelid, and remove the index finger from the lower eyelid.

• The patient should then blink the eye a few times, which helps spread the Nedocromil sodium solution.

• The patient then closes the eye for two to three minutes and then further tips the head down as looking at the floor.

• Placing the finger over the tear duct present on the eye and nose junction, apply gentle pressure.

• Remove the extra solution over the face with a clean tissue.

• If the patient has to use more than one drop in the eye, then the patient should wait for at least five minutes to instill the next drop.

• The patient should tightly close the cap of the dropper bottle.

• Avoid rinsing the dropper tip, and the patient should wash their hand afterward.

What Are the Precautions While Using the Nedocromil Eye Drops?

Precautions are:

• The patient should inform the doctor about the allergic reactions that occur on using Nedocromil eye drops.

• The patient should inform the doctor about the medications taken on regular bases.

• The patient should inform about wearing contact lenses when the eyes are red and itchy.

What if the Patient Forgets the Scheduled Dose?

If the patient forgets to instill the Nedocromil sodium solution or misses the dose, then the patient should instill it soon upon remembering, but if the timing of the next dose is near, then the patient should skip the previous dose and go to the next dose without doubling the dose. The patient should avoid instilling a double dose to complete the missed dose.

What Are the Side Effects of Nedocromil Sodium Solution?

Side effects of Nedocromil sodium are:

• Stinging or burning sensation in the eye.

• Blurred vision.

• Sometimes, increased itchiness or eye redness.

How to Store and Dispose of the Medication?

The storage of the Nedocromil sodium is done in tight containers. It is stored at room temperature and away from moisture and heat. It is kept in a place where children cannot reach.

The unrequired medicine is disposed of in a very special way to prevent any pet, child, or person from having a medicine unknowingly. Avoid the medicine to flush it in the toilet or throw it anywhere. Special take-back programs are provided to dispose of the medicine safely. Even the FDA (Food and Drug Administration) has provided the information on their sites to dispose of the medicine.

For Doctors:

Nedocromil Sodium Ophthalmic Solution:

Nedocromil Sodium Ophthalmic solution is a clear, yellow, sterile solution that is used topically only. It has a chemical name 4H-Pyrano[3,2-g] quinolone-2, 8-dicarboxylic acid, 9-ethyl-6, 9-dihydro-4, 6-dioxo-10-propyl-, disodium salt. It has a chemical formula C19H15NNa2O7 with a molecular weight of 415.30. In each milliliter of Nedocromil sodium, there is an active ingredient of Nedocromil sodium 20 milligrams (2 percent), a preservative Benzalkonium chloride 0.01 percent, and inactive ingredients like sodium chloride 0.5 percent, Edetate disodium 0.05 percent with purified water in it. The solution has a pH of 4.0 to 5.5.

What Are the Indications and Usage of Nedocromil Sodium?

Nedocromil sodium is indicated to treat itchy or allergic conjunctivitis.

What Is the Clinical Pharmacology of Nedocromil Sodium?

• Pharmacodynamics: Nedocromil is an anti-inflammatory agent that is delivered directly to the bronchial mucosa. It shows inhibitory effects on the allergens that are induced in early and late asthmatic and bronchial reactions.

• Mechanism of Action: Nedocromil shows in vitro activation of mediators released from a variety of inflammatory cells that are associated with asthma. Some of the cells are eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Nedocromil here blocks the activation and release of inflammatory mediators such as histamine, prostaglandin, and leukotrienes into the lumen and mucosa of the bronchial. These mediators are derived from arachidonic acid metabolism formed by lipoxygenase and cyclo-oxygenase pathways followed. The mechanism of Nedocromil causes inhibition of axon reflexes and release of sensory neuropeptides like substance P, neurokinin A, and calcitonin peptides. All this results in the blocking of bronchoconstriction.

Pharmacokinetics and Bioavailability:

• Absorption: Nedocromil Sodium shows low systemic absorption. Absorption is mainly by the nasolacrimal duct and not through the conjunctiva.

• The Volume of Distribution: It is not available.

• Protein Binding: Nearly 89 percent of protein is bound in human plasma with a concentration of 0.5 to 50 milligrams per milliliter.

• Metabolism: Nedocromil is not metabolized after intravenous administration and hence excreted unchanged.

• Route of Elimination: As it is not metabolized, it is eliminated primarily unchanged in the urine, nearly 70 percent, and in feces, 30 percent.

• Half-life: It is approximately 3.3 hours.

• Clearance: It is not available.

What Are the Nonclinical Toxicology of Nedocromil Sodium?

The nonclinical toxicology of Nedocromil sodium is as follows:

• Carcinogenesis: Carcinogenic effects were not seen in the studies done on animals. The study done on Wistar rats contained a Nedocromil sodium 24 milligrams per kilogram per day, delivered nearly 400 times more than the human recommended dose. But no studies on humans have been done till now.

• Mutagenesis: No mutagenic effects have been seen on the animals studied. But no studies on humans have been performed to know the mutagenicity. The study with Ames Salmonella assay in mouse Saccharomyces cerevisiae has shown a mitotic gene conversion.

• Impairment of Fertility: The studies performed on animals have shown no effects on male and female reproductive organs or any changes in fertility.

Dosage and Administration:

• Dosage Form: Solution.

• Dosage Strength: 2 %; 5 milliliters in 10 milliliters bottles.

• Recommended Dosage: It is recommended to have one to two drops in each eye twice a day.

• The treatment is continued throughout the period of exposure, usually when the pollen seasons are over or exposure to the offending allergen is terminated, even when the symptoms are absent.

Adverse Reactions:

Some of the common adverse effects seen are:

• Headache.

• Ocular burning.

• Irritation.

• Stinging.

• Unpleasant taste.

• Nasal congestion.

Some of the less common effects include:

• Asthma.

• Conjunctivitis.

• Eye redness.

• Photophobia.

• Rhinitis.

How Is It Supplied?

Nedocromil sodium is supplied as a five-milliliter solution in a natural, low-density polyethylene round eye drop bottle with a controlled dropper tip and a natural propylene cap. It is supplied as a natural, low-density polyethylene round eye drop bottle with a dropper having a controlled tip attached to a natural polypropylene cap.

How Is Nedocromil Sodium Stored?

It is stored at room temperature, usually between 2 degrees to 25 degrees Celsius. And out of reach of children.

Drug Interactions:

• Abacavir: Nedocromil can reduce the excretion of Abacavir, which could result in higher serum levels.

• Aceclofenac: Aceclofenac can decrease the excretion of the Nedocromil and hence increase the serum levels.

• Acetaminophen: Acetaminophen can decrease the excretion of Nedocromil, thus resulting in high serum levels.

• Acyclovir: It also decreases the excretion rate of Nedocromil and results in high serum levels.

What if the Nedocromil Sodium Gets Overdosed?

Nedocromil sodium gets overdosed when it is swallowed mistakenly. If such a thing occurs, it can cause harmful effects. Some of the serious effects are troublesome breathing, and during it serious medical attention is required by the patient immediately upon swallowing it and showing symptoms.

Information for Patients:

• It is important to wash hands thoroughly before and after the use of the medicine.

• Avoid placing the medicine directly over the cornea; instead, try to drop the solution over the lower eyelid.

• Do not touch the doppler tip to the eyes or fingers.

• The medicine should be stored at 2 to 25 degree Celsius.

• Tighten the cap of the bottle and keep it away from children.

• Avoid using the medicine with other ophthalmic drops unless it is being prescribed by the doctor.

Clinical Trials:

• Safety and Efficacy of the Nedocromil Sodium Ophthalmic Solution for 2 %:

The multicenter, open-label evaluation of 1098 patients who were already suffering from ocular itching and had a history of seasonal allergic conjunctivitis. These patients were treated with Nedocromil sodium solution 2 % instilled one drop twice daily in each eye. The patient ocular signs and symptoms were also assessed at baseline, and after one month, the satisfaction score along with adverse effects were all noted. And all patients have shown improvement from the baseline with severity scores for the events like itchiness, burning and stinging sensation, watering, swelling, and tired eyes. It has also shown gritty sensation, eye pain, and light sensitivity. A significant reduction in bulbar conjunctiva with redness and swelling has been reported. Two-thirds of the patients reported with 75 % improvement in the condition after one-month usage of Nedocromil sodium solution of 2 %. However, a few patients also lead to discontinuation because of common adverse effects like burning, unpleasant taste, and headache. The patient also has reported improvement in their daily activities. However, 65 % of the patient was more satisfied with the Nedocromil sodium solution. Hence, the usage of Nedocromil sodium solution of 2 % twice a day was safe and effective for patients suffering from allergic conjunctivitis.